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  3. AKT inhibitor VIII

AKT inhibitor VIII (Synonyms: AKTi-1/2)

Cat. No.: HY-10355 Purity: 98.02%
Handling Instructions

AKT inhibitor VIII (AKTi-1/2) is a cell-permeable quinoxaline compound that has been shown to potently, selectively, allosterically, and reversibly inhibit Akt1, Akt2, and Akt3 activity with IC50s of 58 nM, 210 nM, and 2119 nM, respectively.

For research use only. We do not sell to patients.

AKT inhibitor VIII Chemical Structure

AKT inhibitor VIII Chemical Structure

CAS No. : 612847-09-3

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 146 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
50 mg USD 540 In-stock
Estimated Time of Arrival: December 31
100 mg USD 780 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 11 publication(s) in Google Scholar

Other Forms of AKT inhibitor VIII:

Top Publications Citing Use of Products

    AKT inhibitor VIII purchased from MCE. Usage Cited in: Cell Death Dis. 2017 May 25;8(5):e2817.

    Injury-induced follicular activation is blocked by the mTOR inhibitor rapamycin. Mice are treated with specific inhibitors of the signaling pathways 12 h before surgery and another injection is given just after the surgery. Ovaries are collected at 6 h or 3 weeks after the surgery. C, control ovaries; S, surgically treated ovaries; Rapamycin, mTORC1 inhibitor; Akt VIII, Akt inhibitor; U0126, MAPK inhibitor. Specific inhibition of corresponding signaling pathways by inhibitors. Ovaries are collec

    AKT inhibitor VIII purchased from MCE. Usage Cited in: Nutrients. 2018 Sep 23;10(10). pii: E1366.

    Competition tests of SC79, PHT-427, AT7867, and AKT inhibitor VIII with the CGA probe against enriched AKT by CGA-modified functionalized MMs. Bands of AKT are detected by Western blot.

    View All Akt Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    AKT inhibitor VIII (AKTi-1/2) is a cell-permeable quinoxaline compound that has been shown to potently, selectively, allosterically, and reversibly inhibit Akt1, Akt2, and Akt3 activity with IC50s of 58 nM, 210 nM, and 2119 nM, respectively.

    IC50 & Target[1]

    Akt1

    58 nM (IC50)

    Akt2

    210 nM (IC50)

    Akt3

    2119 nM (IC50)

    In Vitro

    When LnCaP cells are pretreated with AKT inhibitor VIII and then incubated with TRAIL, a dramatic increase in caspase-3 activity (6-10-fold relative to control or TRAIL alone) is observed. This sensitization of tumor cell lines with AKT inhibitor VIII is not limited to LnCaP cells as similar apoptosis induction is observed in HT29, MCF7, and A2780 cells, among others, with chemosensitizers such as camptothecin, herceptin, and doxorubicin[1]. The furanodiene-induced decrease of p-Akt and Akt expressions is enhanced by the Akt inhibitor VIII pretreatment. Furthermore, the furanodiene-induced PARP cleavage is enhanced by Akt inhibitor VIII pretreatment. The Akt inhibitor VIII shows no effect on cleaved PARP expression but decreases the p-Akt and Akt expressions[2]. AKT inhibitor VIII decreases cell viability and increases phosphatidylserine (PS) translocation to the outer leaflet of the plasma membrane, DNA fragmentation, Caspase-9 cleavage, Caspase-3 activation and PARP proteolysis in hESC lines WA01 (H1) and WA09 (H9) and in a hiPSCs cell line generated in our laboratory (FN2.1)[3].

    In Vivo

    Mice are dosed with AKT inhibitor VIII (50 mpk, 3 doses, ip, every 90 min) achieving plasma concentrations of 1.5-2.0 μM, and then the animals are tail vein injected with IGF to stimulate Akt phosphorylation. By IP Western, both basal and IGF stimulated Akt1 and Akt2 phosphorylation are inhibited in mouse lung, with no effect on Akt3 phosphorylation[1].

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 20 mg/mL (36.26 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8128 mL 9.0639 mL 18.1278 mL
    5 mM 0.3626 mL 1.8128 mL 3.6256 mL
    10 mM 0.1813 mL 0.9064 mL 1.8128 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2 mg/mL (3.63 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2 mg/mL (3.63 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [3]

    PSC are plated onto Matrigel coated 96-well plates at densities between 1×103-3×105 cells per well and grown until confluence. 24 hours post-treatments, 50 μg/well of activated 2,3-bis (2-methoxy-4-nitro-5-sulfophenyl)-5 [(phenylamino) carbonyl]-2 H-tetrazolium hydroxide(XTT) in PBS containing 0.3 μg/well of N-methyl dibenzopyrazine methyl sulfate (PMS) are added (final volume 100 μL) and incubated for 1-2 hours at 37°C. Cellular metabolic activity is determined spectrophotometrically at 450 nm.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    551.64

    Formula

    C₃₄H₂₉N₇O

    CAS No.

    612847-09-3

    SMILES

    O=C1NC2=CC=CC=C2N1C3CCN(CC4=CC=C(C5=NC6=CC(NC=N7)=C7C=C6N=C5C8=CC=CC=C8)C=C4)CC3

    Shipping

    Room temperature in continental US; may vary elsewhere

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    Product Name:
    AKT inhibitor VIII
    Cat. No.:
    HY-10355
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    AKT inhibitor VIII

    Cat. No.: HY-10355